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MilliporeSigma™ Calbiochem™ Rad6 Inhibitor, TZ9

Catalog No. 5006550001 Shop All MilliporeSigma Products
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50-065-50001 10 mg
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Catalog No. 50-065-50001 Supplier MilliporeSigma™ Supplier No. 5006550001
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Description

Rad6 Inhibitor, TZ9, CAS 002789-86-7, is a cell-permeable inhibitor of Rad6B-Ub thioester bond formation and subsequent substrate ubiquitination. Directly binds to the catalytic site of Rad6B/HHR6B.

A cell-permeable triazine compound that directly targets human E2 Ubiquitin-conjugating enzyme Rad6B/HHR6B catalytic site via noncovalent interactions and effectively inhibits Rad6B-Ub thioester bond formation as well as subsequent substrate ubiquitination without affecting UbcH5B/UBE2D2-catalyzed BCA2 ubiquitination. Shown to inhibit the proliferation of high Rad6B-expressing MDA-MB-231 (IC50 = 6μM in 72 h), but not the low Rad6B-expressing, non-transformed MCF10A, via G2/M arrest and apoptosis induction. Two known cellular Rad6 substrates, β-catenin and PCNA, are reported to be downregulated following 24 h inhibitor treatment in MDA-MB-231 cultures (0.5 to 5μM).
TRUSTED_SUSTAINABILITY

Specifications

Color Pale Yellow
Description 99% by HPLC
Target Proteins Rad6B/HHR6B
Molecular Formula C17H14N6O4
Solubility DMSO
Form Solid
Quantity 10 mg
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